比咯苯偶氮駢(pyrrolo[2,1-c][1,4]benzodiazpines , PBDs)是鏈球菌屬所分離出來的一種很強的抗癌烷化試劑和基因導向試劑。另一種藥物烯雙炔(enediyne)主要是鏈球菌之代謝物所分離出來的,其生物活性主要來自於雙電子中間體所產生的特定形式。 在本論文中,我們報告設計與合成PBD-enediyne混成試劑,這類混成試劑的合成主要是運用DC-81來聯接多樣性之enediyne。在這8個PBD-enediyne結合中,所獲得產率在2.6% 至9.8%。
pyrrolo[2,1-c][1,4]benzodiazpines (PBDs) are a group of potent naturally occurring antitumor alkylating agents produced by Streptomyces species.Enediyne was either isolated or derived from Streptomyces, which are sourced from a specific generation mode of diradical intermediates. In this thesis, we report the design and synthesis of PBD-enediyne conjugate agents. The synthesis of these conjugates was carried out of DC-81 coupled with a variety of enediyne. There were 8 PBD-enediyne conjugates obtained in 2.6% ~ 9.8% yields.